CN108201525A - A kind of promotion Montelukast Sodium intranasal sorbefacient and its application method - Google Patents
A kind of promotion Montelukast Sodium intranasal sorbefacient and its application method Download PDFInfo
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- CN108201525A CN108201525A CN201711340753.7A CN201711340753A CN108201525A CN 108201525 A CN108201525 A CN 108201525A CN 201711340753 A CN201711340753 A CN 201711340753A CN 108201525 A CN108201525 A CN 108201525A
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- Prior art keywords
- intranasal
- sodium
- sorbefacient
- montelukast sodium
- promotion
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
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- Pharmacology & Pharmacy (AREA)
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- Oil, Petroleum & Natural Gas (AREA)
- Otolaryngology (AREA)
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Abstract
The invention belongs to medicine and pharmacology technical fields, disclose a kind of promotion Montelukast Sodium intranasal sorbefacient and its application method, and the promotion Montelukast Sodium intranasal sorbefacient uses Tween 80：1.0%~10% or sodium caprate：0.2~2.0% or sodium taurocholate：0.1%~1.0%；Promote Montelukast Sodium intranasal sorbefacient application method as above-mentioned accelerating agent is taken to be codissolved in that the use of nose administration dosage form is made in appropriate purified water or in semisolid matrix alone or in combination with Montelukast Sodium.By the present invention in that improve the bioavilability of Montelukast Sodium intranasal absorption with the method for sorbefacient, the auxiliary material that the drug intranasal can be promoted to absorb and the concentration range used are filtered out, the degree of Montelukast Sodium nose administration absorption is improved, the research and development for nose administration dosage form provide foundation.
Description
Technical field
The invention belongs to medicine and pharmacology technical field more particularly to it is a kind of promotion Montelukast Sodium intranasal sorbefacient and its
Application method
Background technology
Montelukast Sodium is a kind of selective leukotriene receptor antagonists, can specificity inhibit cysteinyl leukotriene by
Body has effect to the teiology of inflammation, allergic reaction and asthma, for the prevention and long-term treatment with childhood asthma of being grown up, packet
The asthma symptoms at prevention daytime and night are included, treat the asthma to aspirin-sensitive, bronchoconstriction caused by prevention movement
Deng.
Nose administration is clinically important administering mode.Drug nose administration can avoid the wound of drug administration by injection, avoid baby
The difficulties such as child's oral ingestion is inconvenient and coma patient cannot take orally, and medicine-feeding part is drug absorption position, drug absorption
After can avoid liver first-pass effect, drug quickly enters blood circulation, is conducive to first aid；Nose administration non-invasive, dosage are adjusted
And it is easy to use, to that cannot take orally patient or be difficult to oral infant and drug is extremely advantageous, it can accomplish dosage standard
Really, ensure drug safety.Presently commercially available Montelukast Sodium drug formulation has only tablet and children's tablet and granule, there is no
Nose administration dosage form is applied to clinic.
However, the experimental results showed that, the absorption of Montelukast Sodium intranasal itself is few, is the bad absorption site of the drug,
Therefore the nose administration dosage form of Montelukast Sodium is successfully developed, improves permeability of the Nasal Epithelial Cells to Montelukast Sodium
It is the key that Montelukast Sodium nose administration dosage form is successfully researched and developed and clinical practice.The use of accelerating agent is to improve drug intranasal to absorb
The common method of transhipment that is, by adding in a certain amount of other auxiliary materials i.e. sorbefacient in preparation prescription, changes Drug
The permeability of matter or drug absorption position epithelial cell reaches what drug was effectively treated so as to improve drug absorption bioavilability
Purpose.
In conclusion problem of the existing technology is：Which accelerating agent can effectively facilitate Montelukast Sodium through schneiderian membrane
Epithelial cell absorbs and uses concentration range unknown.Research finds Tween 80, sodium caprate, sodium taurocholate and in certain concentration
The speed and degree that range is absorbed using Montelukast Sodium intranasal is remarkably improved, are having for Montelukast Sodium nose administration dosage form
Imitate auxiliary material.
Invention content
In view of the problems of the existing technology, the present invention provides it is a kind of promotion Montelukast Sodium intranasal sorbefacient and
Its application method,
The invention is realized in this way a kind of promotion Montelukast Sodium intranasal sorbefacient, the promotion montelukast
The each component of sodium intranasal sorbefacient is in mass ratio by Tween-80 1.0%~10% or sodium caprate 0.2~2.0% or courage
Sour sodium 0.1%~1.0%, surplus is Montelukast Sodium, water and other formulation ingredients form.
Further, the Tween-80 promoted in Montelukast Sodium intranasal sorbefacient, sodium caprate, sodium taurocholate one
Kind is two or more.
Another object of the present invention is that providing a kind of application method of promotion Montelukast Sodium intranasal sorbefacient is：
Nose administration is made with other formulation ingredients after taking accelerating agent and Montelukast Sodium respectively or being codissolved in purified water
Dosage form.
Further, the application method for promoting Montelukast Sodium intranasal sorbefacient further comprises：
Intranasal is made with other formulation ingredients after taking accelerating agent and Montelukast Sodium respectively or being codissolved in semisolid matrix
Form of administration uses.
Advantages of the present invention and good effect are：It has filtered out the auxiliary material that the drug intranasal can be promoted to absorb and has used dense
Range is spent, i.e., by using sorbefacient Tween-80 1.0%~10% or sodium caprate 0.2~2.0% or sodium taurocholate 0.1%
~1.0%, 1~2 times of the bioavilability of Montelukast Sodium intranasal absorption can be improved, accelerating agent is easy to use, effect is preferable.
Description of the drawings
Fig. 1 be it is provided in an embodiment of the present invention promotion Montelukast Sodium intranasal sorbefacient by rabbit nose administration for plus
Enter the blood concentration and time history of 5% Tween-80 of accelerating agent.
Fig. 2 be it is provided in an embodiment of the present invention promotion Montelukast Sodium intranasal sorbefacient by rabbit nose administration for plus
Enter the blood concentration and time history of 1% sodium caprate of accelerating agent.
Fig. 3 be it is provided in an embodiment of the present invention promotion Montelukast Sodium intranasal sorbefacient by rabbit nose administration for plus
Enter the blood concentration and time history of 1% sodium taurocholate of accelerating agent.
Fig. 4 be it is provided in an embodiment of the present invention promotion Montelukast Sodium intranasal sorbefacient by rabbit nose administration be nothing
The blood concentration and time history of accelerating agent.
Specific embodiment
In order to make the purpose , technical scheme and advantage of the present invention be clearer, with reference to embodiments, to the present invention
It is further elaborated.It should be appreciated that the specific embodiments described herein are merely illustrative of the present invention, it is not used to
Limit the present invention.
Below in conjunction with the accompanying drawings and specific embodiment is further described the application principle of the present invention.
Promotion Montelukast Sodium intranasal sorbefacient provided in an embodiment of the present invention, by
Tween-80：1.0%~10%
Or sodium caprate：0.2~2.0%
Or sodium taurocholate：0.1%~1.0%；Surplus is Montelukast Sodium, water and other formulation ingredients.
It is described promotion Montelukast Sodium intranasal sorbefacient application method be：
Above-mentioned accelerating agent is taken to be codissolved in that nose administration dosage form is made in appropriate purified water alone or in combination with Montelukast Sodium
It uses；
Or it is dispersed in semisolid matrix and the use of nose administration dosage form is made.
As shown in Figure 1, add in the blood concentration and time history of 5% Tween-80 of accelerating agent；
As shown in Fig. 2, add in the blood concentration and time history of 1% sodium caprate of accelerating agent；
As shown in figure 3, add in the blood concentration and time history of 1% sodium taurocholate of accelerating agent；
As shown in figure 4, blood concentration and time history without accelerating agent.
The AUC and bioavilability absorbed using Montelukast Sodium intranasal after accelerating agent is do not add accelerating agent 1~2 times.
Application example
After 5% Tween-80 of accelerating agent, 1% sodium caprate, 1% sodium taurocholate being added in Montelukast Sodium nasal drops, montelukast sodium
By rabbit nose administration blood concentration and time curve as shown in Figures 1 to 4, the area under the curve AUC of 0~3 hour,
Cmax CmaxEtc. pharmacokinetic parameters see the table below.It is using the AUC of Montelukast Sodium intranasal absorption and bioavilability after accelerating agent
Not plus 1~2 times of accelerating agent.
。
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all essences in the present invention
All any modification, equivalent and improvement made within refreshing and principle etc., should all be included in the protection scope of the present invention.
Claims (4)
1. a kind of promotion Montelukast Sodium intranasal sorbefacient, which is characterized in that the promotion Montelukast Sodium intranasal absorbs
The each component of accelerating agent in mass ratio by Tween-80 1.0%~10% or sodium caprate 0.2~2.0% or sodium taurocholate 0.1%~
1.0%, surplus is Montelukast Sodium, water and other formulation ingredients form.
2. promote Montelukast Sodium intranasal sorbefacient as described in claim 1, which is characterized in that the promotion Meng Lusi
Tween-80, sodium caprate, sodium taurocholate in special sodium intranasal sorbefacient are one or more.
3. a kind of application method of promotion Montelukast Sodium intranasal sorbefacient as described in claim 1~2 any one,
It is characterized in that, the application method of the promotion Montelukast Sodium intranasal sorbefacient is：
Nose administration dosage form is made with other formulation ingredients after taking accelerating agent and Montelukast Sodium respectively or being codissolved in purified water.
4. promote the application method of Montelukast Sodium intranasal sorbefacient as claimed in claim 3, which is characterized in that described
The application method of Montelukast Sodium intranasal sorbefacient is promoted to further comprise：
It takes accelerating agent and Montelukast Sodium respectively or is codissolved in semisolid matrix that nose administration agent is made with other formulation ingredients
Type uses.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711340753.7A CN108201525A (en) | 2017-12-14 | 2017-12-14 | A kind of promotion Montelukast Sodium intranasal sorbefacient and its application method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711340753.7A CN108201525A (en) | 2017-12-14 | 2017-12-14 | A kind of promotion Montelukast Sodium intranasal sorbefacient and its application method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108201525A true CN108201525A (en) | 2018-06-26 |
Family
ID=62604708
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711340753.7A Pending CN108201525A (en) | 2017-12-14 | 2017-12-14 | A kind of promotion Montelukast Sodium intranasal sorbefacient and its application method |
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| Country | Link |
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| CN (1) | CN108201525A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015163978A1 (en) * | 2014-04-25 | 2015-10-29 | R.P. Scherer Technologies, Llc | A stable montelukast solution |
| CN106659734A (en) * | 2014-06-03 | 2017-05-10 | Inq制药集团有限公司 | Silicone oil-containing formulations for nasal application |
-
2017
- 2017-12-14 CN CN201711340753.7A patent/CN108201525A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015163978A1 (en) * | 2014-04-25 | 2015-10-29 | R.P. Scherer Technologies, Llc | A stable montelukast solution |
| CN106659734A (en) * | 2014-06-03 | 2017-05-10 | Inq制药集团有限公司 | Silicone oil-containing formulations for nasal application |
Non-Patent Citations (1)
| Title |
|---|
| 曹娅琪: "《孟鲁司特钠经直肠、鼻腔给药的吸收及促进剂对吸收影响的研究》", 4 December 2017 * |
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| PB01 | Publication | ||
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| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180626 |
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| RJ01 | Rejection of invention patent application after publication |